Total and free brain partition coefficients summarizing the pharmacokinetic studies of berzosertib in FVB wild-type, Bcrp1−/−, Mdr1a/b−/−, and Mdr1a/b−/− Bcrp1−/− mice
| I.V. | P.O. | Steady State | ||||||
|---|---|---|---|---|---|---|---|---|
| Wild-Type | Bcrp1−/− | Mdr1a/b−/− | Mdr1a/b−/− Bcrp1−/− | Wild-Type | Mdr1a/b −/− Bcrp1−/− | Wild-Type | Mdr1a/b−/− Bcrp1−/− | |
| Kp,brain | 0.64 | 0.84 | 2.36 | 17.13 | 0.70 | 13.9 | 0.8 | 14.0 |
| Kpuu,brain | 0.011 | 0.019 | 0.044 | 0.3426 | 0.012 | 0.278 | 0.014 | 0.28 |
| DAfree | 1 | 1.73 | 4 | 31.15 | 1 | 23.16 | 1 | 20 |
P.O., oral administration